| 摘要 |
The present invention provides novel paclitaxel analogs, specifically 2", 3" side-chain halogenated cephalomannine of the formula <IMG> wherein, I. (2"R,3"S)-dihalocephalomannine <IMG> II. (2"S,3"R)-dihalocephalomannine <IMG> III. (2"R,3"S)-dihalo-7-epi-cephalomannine <IMG> IV. (2"S,3"R)-dihalo-7-epi-cephalomannine <IMG> (2"y 3"S)-dihalocephalomannine <IMG> R1=H R2=OH (2" R~3"R)-dihalocepha~omannine R ' <IMG> Rt=OH Ri=H (2"'S~3"S)-dihalo-7-epi-cephalomannine Rl-H RZnOH <IMG> (2"R,3"R)-dihalo-7-epi-cephalomannine R _ R~=H Ri=OH <IMG> and X = halogen, which show strong in vitro and in vivo paclitaxel-like efficacy in a variety of tumors.
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